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liposomal bupivacaine + bupivacaine + clonidine + epinephrine + ketorolac
- Development stage
- Phase 4
- Lead developer
- Kootenai Health
- Modality
- Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Periarticular Injection
01
Overview
This multimodal periarticular injection cocktail was developed and studied by Kootenai Health for the management of postoperative pain in patients undergoing total hip and knee arthroplasty. The combination includes liposomal bupivacaine (an extended-release local anesthetic), immediate-release bupivacaine hydrochloride, clonidine (an alpha-2 adrenergic agonist), epinephrine (an alpha and beta-adrenergic agonist), and ketorolac (a nonsteroidal anti-inflammatory drug). The liposomal formulation of bupivacaine (typically Exparel) provides sustained-release analgesia by blocking voltage-gated sodium channels in nerve cells over an extended period, while the immediate-release bupivacaine provides rapid onset of action. Clonidine enhances the analgesic effect, epinephrine acts as a vasoconstrictor to prolong the anesthetic's duration, and ketorolac provides anti-inflammatory and additional analgesic benefits. This specific multimodal approach was evaluated in a Phase 4 clinical trial to compare its efficacy against a ropivacaine-based multimodal cocktail.
- Other names
- liposomal bupivacaine cocktailKootenai Health periarticular injection cocktail
02
Targets
ADRA1A (α1A)ADRA2A (α2A)β-AR (Beta-adrenergic receptor family)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NaV (Voltage-gated sodium channels)ADRA1 (Alpha-1 adrenergic receptor family)ADRB1 (β1)
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